Aritel, 5 mg 30 pcs.

Aritel is a selective beta1 -adrenoblocker with no sympathomimetic activity of its own and has no clinically significant membrane stabilizing properties. Reduces plasma renin activity, reduces myocardial oxygen demand, reduces heart rate (HR) (at rest and under load). It has hypotensive, antiarrhythmic and antianginal effects. By blocking in low doses beta1 -adrenoreceptors of heart, it reduces catecholamine-stimulated formation of cAMP from ATP, decreases intracellular calcium ion current, has negative chrono-, dromo-, batmo- and inotropic effects, inhibits conduction and excitability, reduces myocardial contractility.

The hypotensive effect of Aritel is related to the decrease of the minute blood volume, sympathetic stimulation of peripheral vessels, decrease of renin-angiotensin system activity (important for patients with initial renin hypersecretion), restoration of sensitivity in response to blood pressure (BP) decrease and influence on the central nervous system (CNS). For arterial hypertension the effect comes in 2-5 days, stable effect – in 1-2 months.

The antianginal effect is caused by decrease of myocardial oxygen demand as a result of shortening of heart rate and contractility, prolongation of diastole, improvement of myocardial perfusion. By increasing left ventricular end-diastolic pressure and increasing ventricular muscle fiber stretch, it may increase oxygen demand, especially in patients with chronic heart failure.

. The antiarrhythmic effect is caused by the removal of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of CAMF, arterial hypertension), reduction of the rate of spontaneous excitation of sinus and ectopic pacemakers and delay of atrioventricular (AV) conduction (mainly in the antegrade and, to a lesser extent, in the retrograde direction through the AV node) and through additional pathways.

Indications

Arterial hypertension;

Coronary heart disease: prevention of angina attacks.

Active ingredient

Composition

1 tablet contains:

Active ingredients:

Bisoprolol fumarate 5 mg.

Associates:

Potato starch – 24 mg;

Silicon dioxide colloid (aerosil) – 1.8 mg;

Magnesium stearate – 0.6 mg;

Lactose monohydrate (milk sugar) – 63.1 mg;

Povidone – 4.5 mg;

Microcrystalline cellulose – 21 mg.

How to take, the dosage

Aritel is taken orally, in the morning on an empty stomach, without chewing, 5 mg once. If necessary, the dose is increased to 10 mg once a day. Maximal daily dose is 20 mg/day.
In patients with impaired renal function and creatine clearance less than 20 ml/min or with significant liver dysfunction the maximal daily dose is 10 mg.

Interaction

Allergens used for immunotherapy or allergen extracts for skin testing increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.

Iodine-containing intravenous radiopaque drugs increase the risk of anaphylactic reactions.

Phenytoin when administered intravenously, drugs for inhaled general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressant effects and the likelihood of BP reduction.

Aritel alters the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased BP). Reduces clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentrations, especially in patients with initially increased clearance of theophylline under the influence of smoking.
Hypotensive effect is weakened by nonsteroidal anti-inflammatory drugs (Na+ retention and blockade of prostaglandin synthesis by kidneys), glucocorticosteroids and estrogens (Na+ ion retention).

Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), amiodorone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV blockade, cardiac arrest, and heart failure.

Nifedipine can lead to a significant decrease in BP.

Diuretics, clonidine, sympatholytics, hydralazine and other hypotensive drugs may lead to an excessive decrease in BP.

Longens the effects of non-depolarizing myorelaxants and the anticoagulant effect of coumarins.

Tricyclic and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and sleeping pills increase CNS depression.

The concomitant use with MAO inhibitors is not recommended due to a significant increase in hypotensive effect, a break in treatment between MAO inhibitors and bisoprolol should be at least 14 days.

Unhydrogenated ergot alkaloids increase the risk of peripheral circulatory disorders.

Ergotamine increases the risk of peripheral circulation disorders; sulfasalazine increases bisoprolol plasma concentrations; rifampicin shortens the elimination half-life.

Special Instructions

Control of patients taking Aritel should include measurement of HR and BP (at the beginning of treatment – daily, then once every 3-4 months), ECG, determination of blood glucose in diabetic patients (once every 4-5 months). In elderly patients it is recommended to monitor kidney function (once every 4-5 months).

Before starting treatment, it is recommended to conduct a study of external respiratory function in patients with a history of complicated bronchopulmonary disease.

If clonidine is taken at the same time, its administration can be discontinued only after several days after discontinuation of Aritel.

Contraindications

Hypersensitivity to drug components and other beta-adrenoblockers,

Shock (including cardiogenic);

Collapse;

Pulmonary edema;

Acute heart failure, decompensated chronic heart failure, AV block II-III degree., Sinoatrial block, sinus node weakness syndrome, severe bradycardia, Prinzmetal angina, cardiomegaly (without signs of heart failure), arterial hypotension (systolic BP less than 100 mmHg, especially in myocardial infarction);

Bronchial asthma and chronic obstructive pulmonary disease in the history;

Concurrent use of monoamine oxidase inhibitors (MAOIs) (except MAO-B);

Late stages of peripheral circulatory disorders, Raynaud’s disease);

Pheochromocytoma (without concurrent use of alpha-adrenoblockers);

Metabolic acidosis;

Age

Side effects

Central nervous system: increased fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia, paresthesias in the extremities (in patients with “intermittent” claudication and Raynaud’s syndrome), tremor.

Sensory organs: visual impairment, decreased secretion of lacrimal fluid, dry and painful eyes, conjunctivitis.

Cardiovascular system side: sinus bradycardia, palpitations, myocardial conduction disturbances, AV blockade (up to development of complete transverse blockade and cardiac arrest), arrhythmias, weakened myocardial contractility, development (aggravation) of chronic heart failure (swelling of ankles, feet; dyspnea), BP decrease, orthostatic hypotension, manifestation of angiospasm (worsening of peripheral circulatory disorders, coldness of the lower extremities, Raynaud’s syndrome), chest pain.

From the digestive system: Dry oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, disorders of liver function (dark urine, jaundice of sclerae or skin, cholestasis), changes in taste.

The respiratory system: nasal congestion, difficulty in breathing when prescribed in high doses (loss of selectivity) and/or in predisposed patients – laryngo- and bronchospasm.
Endocrine system: hyperglycemia (in patients with insulin-independent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroidism.

Allergic reactions: itching, rash, urticaria.

Skin reactions:increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms.

Laboratory findings:thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in liver enzyme activity (increased ALT, AST), bilirubin levels, triglycerides.

Fetal effects: intrauterine growth retardation, hypoglycemia, bradycardia.

Others:back pain, arthralgia, decreased libido, decreased potency, withdrawal syndrome (increased angina pectoris attacks, increased BP).

Overdose

Symptoms: arrhythmia, ventricular extrasystole, marked bradycardia, AV blockade, marked BP decrease, chronic heart failure, cyanosis of finger nails or palms, difficulty breathing, bronchospasm, dizziness, fainting, seizures.

Treatment: gastric lavage and administration of adsorptive drugs; symptomatic therapy: if AV blockade developed – intravenous (IV) 1-2 mg of atropine, epinephrine or placement of a temporary pacemaker; if ventricular extrasystole – lidocaine (Class Ia drugs are not used ); if BP decreases – the patient should be in Trendelenburg position; If there are no signs of pulmonary edema – intravenous plasma exchange solutions, if ineffective – administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and to eliminate marked BP decrease); in heart failure – cardiac glycosides, diuretics, glucagon; in convulsions – intravenous diazepam; in bronchospasm – beta2-adreno stimulants inhaled.

Similarities